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Assay Detail

CHEMBL4146208

Review assay metadata, readout intent, target linkage, and publication context from the same page.

Functional
Antiproliferative activity against human NCI-H3122 cells after 72 hrs by SRB or CCK8 assay
22
Total Activities
22
Compounds Tested
1
Activity Types
0
Assay Parameters

Assay Information

Assay Type Functional
Organism Homo sapiens
Cell Type NCI-H3122
Confidence 1 — Organism
Curated By Intermediate

Target

NCI-H3122 (CHEMBL4296475)
Type CELL-LINE
Organism Homo sapiens

Publication

Discovery of 2,4-diarylaminopyrimidines bearing a resorcinol motif as novel ALK inhibitors to overcome the G1202R resistant mutation.
Geng K, Xia Z, Ji Y, Zhang RR, Sun D, Ai J, Song Z, Geng M, Zhang A.
Eur J Med Chem (2018) 144 : 386 -397
PubMed 29288940 · DOI

Activity Statistics

Type Count Avg pChEMBL Best pChEMBL
IC50 22 7.47 8.40

Compounds Tested

Compound Name Phase Activities Best pChEMBL
CHEMBL4168049 1 8.40
CHEMBL4172925 1 8.17
CHEMBL4168868 1 8.16
CHEMBL4177038 1 8.14
CHEMBL3286830 LORLATINIB 4.0 1 8.11
CHEMBL4175908 1 8.04
CHEMBL4162661 1 7.89
CHEMBL4170592 1 7.86
CHEMBL4174031 1 7.24
CHEMBL4168701 1 7.19
CHEMBL4170213 1 7.16
CHEMBL4162295 1 7.08
CHEMBL2403108 CERITINIB 4.0 1 7.02
CHEMBL3357439 1 7.01
CHEMBL4172048 1 7.00
CHEMBL4176561 1 6.91
CHEMBL4169529 1 6.59
CHEMBL601719 CRIZOTINIB 4.0 1 6.52
CHEMBL4166111 1 -
CHEMBL4177392 1 -
CHEMBL4162252 1 -
CHEMBL4161453 1 -

Activity Data

Compound Name Type Rel. Value Units pChEMBL
CHEMBL4168049 IC50 = 4.0 nM 8.40
CHEMBL4172925 IC50 = 6.8 nM 8.17
CHEMBL4168868 IC50 = 6.9 nM 8.16
CHEMBL4177038 IC50 = 7.2 nM 8.14
CHEMBL3286830 LORLATINIB IC50 = 7.8 nM 8.11
CHEMBL4175908 IC50 = 9.1 nM 8.04
CHEMBL4162661 IC50 = 12.8 nM 7.89
CHEMBL4170592 IC50 = 13.7 nM 7.86
CHEMBL4174031 IC50 = 57.0 nM 7.24
CHEMBL4168701 IC50 = 64.0 nM 7.19
CHEMBL4170213 IC50 = 69.0 nM 7.16
CHEMBL4162295 IC50 = 84.0 nM 7.08
CHEMBL2403108 CERITINIB IC50 = 96.0 nM 7.02
CHEMBL3357439 IC50 = 97.0 nM 7.01
CHEMBL4172048 IC50 = 99.0 nM 7.00
CHEMBL4176561 IC50 = 123.0 nM 6.91
CHEMBL4169529 IC50 = 254.0 nM 6.59
CHEMBL601719 CRIZOTINIB IC50 = 303.0 nM 6.52
CHEMBL4166111 IC50 > 1000.0 nM -
CHEMBL4177392 IC50 > 1000.0 nM -
CHEMBL4162252 IC50 > 1000.0 nM -
CHEMBL4161453 IC50 > 1000.0 nM -